More sensitive and specific methods for early detection are imperative to improve survival rates in oral cancer. However, oral cancer detection is still largely based on visual examination and histopathology of biopsy material, offering no molecular selectivity or spatial resolution. Intuitively, the addition of optical contrast could improve oral cancer detection and delineation. Our fluorescently labeled small molecule inhibitor PARPi-FL binds to the DNA repair enzyme PARP1 and is a potential diagnostic aid for oral cancer delineation. Recently, our most advanced optically active PARP imaging probe, PARPi-FL, has advanced to a phase I/II clinical trial and will be evaluated as a contrast agent for oral cancer imaging (NCT03085147). In short, 1) PARP1 is highly overexpressed in human oral cancer biospecimen, 2) PARPi-FL accumulated with high specificity in PARP1 expressing oral cancer xenografts, and 3) oral cancer imaging is also feasible when PARPi-FL is applied topically instead of intravenously. We will also compare the potential benefits of our molecularly targeted PARPi-FL guided imaging approach in comparison to existing oral cancer screening adjuncts and mention the adaptability of PARPi-FL imaging to other environments and tumor types.
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